1. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease MAPK/ERK Pathway Stem Cell/Wnt TGF-beta/Smad Immunology/Inflammation NF-κB
  2. PPAR ERK JNK TGF-beta/Smad NO Synthase COX NF-κB Interleukin Related
  3. Lobeglitazone sulfate

Lobeglitazone sulfate is a new type of thiazolidinedione. Lobeglitazone sulfate is the orally active agonist for PPAR with EC50 of 137.4 nM and 546.3 nM for PPARγ and PPARα. Lobeglitazone sulfate is the inhibitor for ERK/JNK/Smad/NF-κB signaling pathway. Lobeglitazone sulfate exhibits anti-inflammatory, anti-diabetic, anti-fibrotic and anti-atherosclerotic properties.

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Lobeglitazone sulfate

Lobeglitazone sulfate 構造式

CAS 番号 : 763108-62-9

容量 価格(税別) 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 255 在庫あり
Solution
10 mM * 1 mL in DMSO USD 255 在庫あり
Solid
5 mg $200 在庫あり
10 mg $320 在庫あり
25 mg $510 在庫あり
50 mg $765 在庫あり
100 mg $1115 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 0 publication(s) in Google Scholar

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製品説明

Lobeglitazone sulfate is a new type of thiazolidinedione. Lobeglitazone sulfate is the orally active agonist for PPAR with EC50 of 137.4 nM and 546.3 nM for PPARγ and PPARα. Lobeglitazone sulfate is the inhibitor for ERK/JNK/Smad/NF-κB signaling pathway. Lobeglitazone sulfate exhibits anti-inflammatory, anti-diabetic, anti-fibrotic and anti-atherosclerotic properties[1][2][3][4][5][6].

IC50 & Target

PPARγ

137.4 nM (EC50)

PPARα

546.3 nM (EC50)

体外実験

Lobeglitazone sulfate increases glucose uptake in 3T3-L1 adipocytes and L6 muscle cells[1].
Lobeglitazone sulfate (50-200 μM, 24 h) inhibits NO generation and the expressions of pro-inflammtory cytokines like IL-1β, IL-6, iNOS, COX-2 and MCP-1 in LPS (HY-D1056)-stimulated BMDMs[2].
Lobeglitazone sulfate (10 μM, 48 h) inhibits TGF-β1-induced expression of α-SMA and fibronectin, inhibits Smad signaling pathway in primary human corneal fibroblast, and exhibits anti-fibrotic property[3].
Lobeglitazone sulfate (1-15 μM, 24 h) inhibits PDGF-induced proliferation and migration of vascular smooth muscle cells (VSMCs), inhibits TNF-α-induced NF-κB p65 translocation[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Real Time qPCR[2]

Cell Line: BMDM
Concentration: 50-200 µM
Incubation Time: 24 h
Result: Inhibited the expression of IL-1β, IL-6, iNOS, COX-2 and MCP-1.

Western Blot Analysis[2]

Cell Line: primary human corneal fibroblast
Concentration: 1-10 µM
Incubation Time: 48 h
Result: Inhibited expression of α-SMA and fibronectin.
体内実験

Lobeglitazone sulfate (1-10 mg/kg, po for 8 weeks) exhibits anti-atherosclerotic property in ApoE / mouse models[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: ApoE−/− mouse aortic atherosclerosis models[4]
Dosage: 1-10 mg/kg
Administration: po for 8 weeks
Result: Reduced aortic arch plaques.
臨床実験
分子量

578.61

分子式

C24H26N4O9S2

CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C(SC1CC2=CC=C(C=C2)OCCN(C)C3=NC=NC(OC4=CC=C(C=C4)OC)=C3)NC1=O.O=S(O)(O)=O

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶剤 & 溶解度
体外: 

DMSO : 25 mg/mL (43.21 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7283 mL 8.6414 mL 17.2828 mL
5 mM 0.3457 mL 1.7283 mL 3.4566 mL
10 mM 0.1728 mL 0.8641 mL 1.7283 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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一般には略語で表示されます:C1V1 = C2V2

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純度とドキュメンテーション
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7283 mL 8.6414 mL 17.2828 mL 43.2070 mL
5 mM 0.3457 mL 1.7283 mL 3.4566 mL 8.6414 mL
10 mM 0.1728 mL 0.8641 mL 1.7283 mL 4.3207 mL
15 mM 0.1152 mL 0.5761 mL 1.1522 mL 2.8805 mL
20 mM 0.0864 mL 0.4321 mL 0.8641 mL 2.1603 mL
25 mM 0.0691 mL 0.3457 mL 0.6913 mL 1.7283 mL
30 mM 0.0576 mL 0.2880 mL 0.5761 mL 1.4402 mL
40 mM 0.0432 mL 0.2160 mL 0.4321 mL 1.0802 mL
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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製品名:
Lobeglitazone sulfate
製品番号:
HY-14928A
数量:
MCE 日本正規代理店: